Kjell Undheim

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Immune reactions to citrulline-containing proteins appear to be central in the immunopathogenesis of rheumatoid arthritis. Citrulline residues are introduced into proteins by deimination of arginine residues, likely by an enzymatic process. There is a need to characterize which proteins in the inflamed joints of rheumatoid patients contain citrulline in(More)
The key construction in the preparation of as-indacene-bridged bis(alpha-amino acid) derivatives was effected by a Ru(II)-catalyzed RCM cascade reaction of appropriately substituted triynes. The latter were available after stepwise and stereocontrolled alkynylations of (2R)-2,5-dihydro-2-isopropyl-3,6-dimethoxypyrazine as chiral auxiliary. The regio- and(More)
The effect of 2-(2-thenyl)sulfonyl-5-bromopyrimidine (NY 4137) on cells of the human line NHIK 3025 was investigated. It was shown that NY 4137 induces cell cycle specific inhibition in metaphase. A dose-dependent prolongation of metaphase was found and the fraction of cells able to escape metaphase arrest declined gradually as the concentration of NY 4137(More)
Two pyrimidine analogs (metahalones) NY 3163, NY 3170 have been tested for their effects on the growth of rat glioma cells in monolayer and in spheroid culture. Both substances have earlier been found to inhibit the microtubule system in malignant cells. In glioma cells, arrest of mitosis was accompanied by repeated cycles of DNA synthesis, leading to(More)
The effect of the two closely related drugs, the sulfone 2-(2-thenyl)sulfonyl-5-bromopyrimidine (NY 4137), and the sulfoxide 2-(2-thenyl)sulfinyl-5-bromopyrimidine (NY 4138), a sulfoxide, on the survival of cells of the human line NHIK 3025 was investigated. Cell survival was measured as the ability of single cells to form macroscopic colonies. Two-hour(More)
The focus has been on the development of methodology for stereoselective preparation of spiroannulated intermediates of the Schöllkopf chiron and further transformations to cyclic alpha-amino acids. The spiroannulations are effected by Ru(II)-catalysed ring-closing metathesis reactions, by Ru(II)- and Pd(0)-catalysed cycloisomerisations, by Rh(II)-carbenoid(More)
Tricarbonylation of clarithromycin has been effected in a one-pot reaction with phosgene. The 11,12-diol moiety was closed into a cyclic carbonate, while the dimethylamino alcohol of the desosamine sugar was cyclised with loss of a methyl group to form a cyclic 2',3'-carbamate. The 4'' hydroxyl group in clarithromycin was converted into a chloroformate(More)
Cyclic adenosine monophosphate (cAMP) has been converted into its 8-bromo derivative and 2'O-TBDMS protected before activation of the phosphoric acid moiety with a reagent generated in situ from oxalyl chloride and DMF. Further reactions with primary amines furnished corresponding phosphoramidates with high stereoselectivity at the phosphorus atom.(More)